382185

HDAC Inhibitor XXII, NCH51

The HDAC Inhibitor XXII, NCH51, also referenced under CAS 848354-66-5, controls the biological activity of HDAC. This small molecule/inhibitor is primarily used for Cell Structure applications.

• 別名: HDAC Inhibitor XXII, NCH51, Thioisobutyric acid(S-(6-(4-phenyl-2-thiazolylcarbamoyl)hexyl) ester
• 実験式（ヒル表記法）: C₂₀H₂₆N₂O₂S₂
• CAS番号: 848354-66-5
• 分子量: 390.56
• MDL番号: MFCD08705329
• UNSPSCコード: 12352200

特性

• 品質水準: 100
• アッセイ: ≥97% (HPLC)
• フォーム: powder
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze
• 色: white
• 溶解性: DMSO: 100 mg/mL
• 輸送温度: ambient
• 保管温度: −20°C
• InChI: 1S/C20H26N2O2S2/c1-15(2)19(24)25-13-9-4-3-8-12-18(23)22-20-21-17(14-26-20)16-10-6-5-7-11-16/h5-7,10-11,14-15H,3-4,8-9,12-13H2,1-2H3,(H,21,22,23)
• InChI Key: MDYDGUOQFUQOGE-UHFFFAOYSA-N

詳細

詳細

A cell-permeable S-isobutyryl prodrug that is processed intracellularly to form the potent HDAC inhibitor NCH-31 (IC50 = 48 and 170 nM, respectively, using partially purified HDAC1 or HeLa nuclear extract) that is predicted to exhibit a similar HADC binding mode as that of SAHA with its sulfhydryl replacing SAHA′s hydroxamate as the active-site zinc-targeting group. NCH-51 is shown to exhibit comparable antiproliferative (mean IC₅₀ = 3.8 µM vs. 3.7 µM for SAHA; 48 h treatment) and apoptotic activity as SAHA against various cancer cell lines, but not PBMCs from 4 healthy individuals (IC₅₀ >30 µM with either drug), and the antioxidant N-Acetyl-L-Cysteine (NAC; Cat. No. 106425) at 2 mM is reported to abolish the cell-growth inhibition caused by either 3 µM NCH-51 or SAHA in the Multiple Myeloma U266 cultures. Half-life in human plasma at 37 °C = 24 h.

A cell-permeable S-isobutyryl prodrug that is processed intracellularly to form the potent HDAC inhibitor NCH-31 (IC50 = 48 and 170 nM, respectively, using partially purified HDAC1 or HeLa nuclear extract) that is predicted to exhibit a similar HADC binding mode as that of SAHA with its sulfhydryl replacing SAHA′s hydroxamate as the active-site zinc-targeting group. NCH-51 is shown to exhibit comparable antiproliferative (mean IC₅₀ = 3.8 µM vs. 3.7 µM for SAHA; 48 h treatment) and apoptotic activity as SAHA against various cancer cell lines, but not PBMCs from 4 healthy individuals (IC₅₀ >30 µM with either drug), and the antioxidant N-Acetyl-L-Cysteine (NAC; Cat. No. 106425) at 2 mM is reported to abolish the cell-growth inhibition caused by either 3 µM NCH-51 or SAHA in the Multiple Myeloma U266 cultures. Half-life in human plasma at 37 °C = 24 h.

警告

Toxicity: Regulatory Review (Z)

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

その他情報

#31: Thiol - 7-Mercaptoheptanoic acid (4-phenyl-2-thiazolyl)amide

Sanda, T., et al. 2007. Leukemia21, 2344.
Suzuki, T., et al. 2007. Bioorg. Med. Chem. Lett.17, 1558.
Suzuki, T., et al. 2005. J. Med. Chem.48, 1019.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable